Steiness E, Rasmussen F, Svendsen O, Nielsen P
Acta Pharmacol Toxicol (Copenh). 1978 May;42(5):357-64. doi: 10.1111/j.1600-0773.1978.tb02217.x.
Serum creatine phosphokinase (CPK) activity has been determined before and after intramuscular injection of lidocaine, diazepam or saline in humans and lidocaine, diazepam, digoxin and saline in pigs and rabbits. Two ml volum of each of the drugs was given to humans as well as to the experimental animals. No changes in CPK activity were found after saline in humans or rabbits but a minor increase was demonstrated in pigs. A marked increase of CPK activity was demonstrated after lidocaine or diazepam in humans and after lidocaine, diazepam or digoxin in pigs and rabbits. Post mortem examination of the injection sites in the animals revealed extensive muscle tissue necrosis after lidocaine, diazepam and digoxin. No damage of the tissue was found after saline. CPK activity was also determined in rabbits receiving 2 ml of dilutions of diazepam in saline. The injection sites were examined post mortem. The CPK activity was increased in animals receiving 1:2 and 1:8 dilutions while a 1:20 dilution did not give rise to changes in the enzyme activity. The necrotic area diminished when diazepam was diluted and no pathological changes were found at the injection sites after the 1:20 dilution. Measuring the CPK activity in rabbits after an intramuscular injection seems to be a sensitive method for the determination of local toxicity.
已测定人体肌肉注射利多卡因、地西泮或生理盐水后，以及猪和兔肌肉注射利多卡因、地西泮、地高辛或生理盐水前后的血清肌酸磷酸激酶（CPK）活性。给人体和实验动物均注射2毫升每种药物。人体或兔注射生理盐水后CPK活性未发现变化，但猪出现轻微升高。人体注射利多卡因或地西泮后，以及猪和兔注射利多卡因、地西泮或地高辛后，CPK活性显著升高。对动物注射部位进行尸检发现，注射利多卡因、地西泮和地高辛后出现广泛的肌肉组织坏死。注射生理盐水后未发现组织损伤。还测定了接受2毫升地西泮生理盐水稀释液的兔的CPK活性，并在尸检时检查了注射部位。接受1:2和1:8稀释液的动物CPK活性升高，而1:20稀释液未引起酶活性变化。地西泮稀释后坏死面积减小，1:20稀释后注射部位未发现病理变化。肌肉注射后测定兔的CPK活性似乎是一种测定局部毒性的灵敏方法。
